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Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

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| Description | Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors. |
| In vitro | Binding studies with [3H]ac-RYYRWK-NH2 on rat cortical membranes identified a single high-affinity binding site (Kd = 0.071 nM). Furthermore, Naloxone benzoylhydrazone competitively inhibited [3H]ac-RYYRWK-NH2 binding to rat cortical membranes (Ki = 104 nM) and to human ORL1 receptors (Ki = 136 nM). It also displaced [125I]Tyr14-NC-OH binding to ORL1 receptors with a Ki of 37 nM, indicating specificity as it showed no affinity for μ-, κ-, or δ-opioid receptors. |
| Synonyms | Ac-RYYRWK-NH2 TFA |
| Molecular Weight | 1126.21 |
| Formula | C51H70F3N15O11 |
| Cas No. | 408305-09-9 |
| Smiles | OC(=O)C(F)(F)F.CC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O |
| Sequence | Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH2.TFA |
| Sequence Short | RYYRWK |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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